title: 1-[2-(2-Methoxyphenylamino)ethylamino]-3-(naphthalene-1-yloxy)propan-2-ol as a potential anticancer drug.
abstract: The aim of the present study was to assess the anticancer effect of several naftopidil analogues on human malignant mesothelioma cell lines NCI-H28, NCI-H2052, NCI-H2452, and MSTO-211H, human lung cancer cell lines A549, SBC-3, and Lu-65, human hepatoma cell lines HepG2 and HuH-7, human gastric cancer cell lines MKN-28 and MKN-45, and human bladder cancer cell lines 253J, 5637, KK-47, TCCSUP, T24, and UM-UC-3, human prostate cancer cell lines DU145, LNCap, and PC-3, and human renal cancer cell lines ACHN, RCC4-VHL, and 786-O. We newly synthesized 21 naftopidil analogues, and of them 1-[2-(2-methoxyphenylamino)ethylamino]-3-(naphthalene-1-yloxy)propan-2-ol (HUHS1015) most efficiently reduced cell viability for all the investigated malignant mesothelioma cell lines in a concentration (1-100 μmol/l)-dependent manner. HUHS1015 reduced cell viability for all other investigated cancer cell lines, to an extent similar to that for malignant mesothelioma cell lines. HUHS1015 activated caspase-3 and -4, without activating caspase-8 and -9, in malignant mesothelioma cell lines. The results of the present study, thus, indicate that HUHS1015 induces apoptosis in a variety of cancer cells, possibly by activating caspase-4 and the effector caspase-3.
authors.affiliation: Division of Bioinformation, Department of Physiology, Hyogo College of Medicine, Nishinomiya, Japan.
authors.forename: Takeshi
authors.initials: T
authors.lastname: Kanno
authors.forename: Akito
authors.initials: A
authors.lastname: Tanaka
authors.forename: Tadashi
authors.initials: T
authors.lastname: Shimizu
authors.forename: Takashi
authors.initials: T
authors.lastname: Nakano
authors.forename: Tomoyuki
authors.initials: T
authors.lastname: Nishizaki
mesh_terms: D000814:Aniline Compounds / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000494:pharmacology*; D020169:Caspases / Q000378:metabolism; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D011412:Propanolamines / Q000494:pharmacology
chemical_list: C586405:1-(2-(2-methoxyphenylamino)ethylamino)-3-(naphthalene-1-yloxy)propan-2-ol; D000814:Aniline Compounds; D000970:Antineoplastic Agents; D011412:Propanolamines; D020169:Caspases